Loading and releasing ciprofloxacin in photoactivatable liposomes

We demonstrate that ciprofloxacin can be actively loaded into liposomes that contain small amounts of porphyrin-phospholipid (PoP). PoP renders the liposomes photoactivatable, so that the antibiotic is released from the carrier under red light irradiation (665 nm). The use of 2 mole % PoP in the liposomes accommodated active loading of ciprofloxacin. Further inclusion of 2 mole % of an unsaturated phospholipid accelerated light-triggered drug release, with more than 90% antibiotic release from the liposomes occurring in less than 30 s. With or without laser treatment, ciprofloxacin PoP liposomes inhibited the growth of Bacillus subtilis in liquid media, apparently due to uptake of the liposomes by the bacteria. However, when liposomes were first separated from smaller molecules with centrifugal filtration, only the filtrate from laser-treated liposomes was bactericidal, confirming effective release of active antibiotic. These results establish the feasibility of remote loading antibiotics into photoactivatable liposomes, which could lead to opportunities for enhanced localized antibiotic therapy.